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Codeine is an opioid medication used to treat mild to moderate pain, suppress coughing, and manage diarrhea. It is a naturally occurring alkaloid found in the opium poppy and is the most commonly used opiate worldwide. 
Key Information
  • Medical Uses: Codeine is primarily used for short-term pain relief, often in combination with non-opioid analgesics like acetaminophen (paracetamol) or ibuprofen for enhanced effect. It also works as an antitussive (cough suppressant) and an antidiarrheal agent.
  • Mechanism of Action: Codeine is a prodrug, meaning it is converted into its active form, primarily morphine, by the enzyme CYP2D6 in the liver. Morphine then binds to opioid receptors in the central nervous system to block pain signals and reduce the cough reflex.
Availability: Availability varies by country and concentration. In many places, including the United States, pure codeine and higher-dose formulations require a prescription and are regulated as controlled substances. Lower-strength combination products may be available over the counter under pharmacist supervision in some regions.Forms: It is available as tablets, oral solutions/syrups, and injections (typically only in a hospital setting). 
Important Considerations and Risks
  • Genetic Variation: The effectiveness and safety of codeine depend on how quickly an individual's body metabolizes it.
    • Poor metabolizers (about 5-10% of some populations) may experience little to no pain relief.
    • Ultra-rapid metabolizers (present in higher percentages in some ethnic groups, such as North Africans) convert codeine into morphine too quickly, which can lead to dangerously high levels of morphine in the body, resulting in serious side effects like respiratory depression or death.